Improvement of Aqueous Solubility of Lapatinib-derived Analogs: Identification of a Quinolinimine as a Lead for Human African Trypanosomiasis Drug Development

Lapatinib, an approved EGFR inhibitor, was explored as a starting point for the synthesis of new hits against Trypanosoma brucei, the causative agent of human African trypanosomiasis (HAT). Previous work culminated in 1 (NEU-1953), which was part of a series typically associated with poor aqueous so...

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Veröffentlicht in:J Med Chem
Hauptverfasser: Bachovchin, Kelly A., Sharma, Amrita, Bag, Seema, Klug, Dana M., Schneider, Katherine M., Singh, Baljinder, Jalani, Hitesh B., Buskes, Melissa J., Mehta, Naimee, Tanghe, Scott, Momper, Jeremiah D., Sciotti, Richard J., Rodriguez, Ana, Mensa-Wilmot, Kojo, Pollastri, Michael P., Ferrins, Lori
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2019
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC6556231/
https://ncbi.nlm.nih.gov/pubmed/30565932
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b01365
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